Cytoskeletal Signaling

<p>KY-02327 acetate inhibits Dvl-CXXC5, stabilizes Wnt/β-catenin signaling, and enhances osteoblast differentiation.</p>

<p>RMS-07, a covalent MPS1/TTK inhibitor, has an IC50 of 13.1 nM, targeting a kinase hinge cysteine.</p>

<p>SR121566A is a novel non-peptide antagonist of Glycoprotein IIb/IIIa (GP IIb-IIIa).</p>

<p>C086 is a novel and potent Hsp90 inhibitor that suppresses cell cycle progression, induces apoptosis, and exhibits anti-metastatic properties by modulating various mechanisms in different cell types.</p>

<p>6-B345TTQ is an α4 integrin inhibitor that can impede the interaction between α4 and Leupaxin. This compound is applicable for studies focused on inflammation research.</p>

<p>MT-134 is a SkMII -specific inhibitor and has excellent exposure in muscles.</p>

<p>Tau ligand-1 (Compound 75) is a ligand of aggregated tau protein that can penetrate the blood-brain barrier. In tissues affected by Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 shows high affinity for aggregated tau protein, with equilibrium dissociation constants (KD) ranging from 1 to 3.8 nM. It holds potential as a positron emission tomography (PET) tracer for imaging studies of tau-related diseases within the central nervous system.</p>

<p>Compound 13m, a difluoro derivative, activates Nrf2/HO-1, showing neuroprotective and antioxidant effects, useful in PD research.</p>

<p>GR 83895 is an antagonist of prototype fibrinogen receptor.</p>

<p>Des-ethyl-carafiban (Compound 44) is an antagonist of the fibrinogen receptor, effectively inhibiting platelet aggregation induced by various agonists. It is useful for research in thrombotic diseases.</p>

<p>POSH-IN-2 (MIDI) is a mitochondrial fission inhibitor and a DRP1 inhibitor that effectively prevents mitochondrial fragmentation caused by cellular stress and genetic mitochondrial damage. It covalently interacts with DRP1-C367 to target the interaction of DRP1 with multiple receptors.</p>

<p>GSK3335103 is a non-peptide, orally active inhibitor of αvβ6 integrin (pIC50=8), employed in the study of pulmonary fibrosis.</p>

<p>FO-4-15 is an activator of mGluR1/CaMKIIα. It exhibits protective effects against H2O2 in human neuroblastoma (SH-SY5Y) cells. In mice with Alzheimer's disease, FO-4-15 enhances cognitive function by activating the mGluR1/CaMKIIα pathway, reducing Aβ accumulation, Tau hyperphosphorylation, and synaptic damage.</p>

<p>NRX-2663 boosts β-catenin binding to E3 ligase SCFβ-TrCP (Kd: 54.8 nM, EC50: 22.9 nM).</p>

<p>Fradafiban binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM. Fradafiban is a non-polypeptide platelet glycoprotein IIb/IIIa antagonist.</p>

<p>Row174336 (compound 29) serves as an efficient inhibitor of the Hsp110-STAT3 interaction, exhibiting antiproliferative activity in the HPAEC cell line with an IC50 of 22.67 μM.</p>

<p>Compound IIc inhibits tubulin polymerization, arrests cell cycle at G2/M in HCT116 cells, IC50 12.7 μM, potential for cancer research.</p>

<p>Ack1 inhibitor 1 is a potent and selective orally active inhibitor of ACK1 kinase, with an IC50 value of 2.1 nM. It effectively inhibits the phosphorylation of ACK1 and the activation of downstream AKT, demonstrating anti-tumor activity [1].</p>

<p>TTBK1/2-IN-3 (compound 10) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 can reduce the expression of primary cilia on the surface of human induced pluripotent stem cells (iPSC).</p>

<p>ETB is a potent inhibitor of Hsp60 chaperone activity. It can impede the chaperone function of both wild-type proteins and the C237A and C447A mutant proteins. ETB binds to Hsp60 at Cys442, and the C442A mutant demonstrates resistance to ETB inhibition.</p>

<p>KAA, an anticancer compound, inhibits centrosome clustering and targets HSET+ yeast and cancer cells.</p>

<p>Tubulin-IN-33, an oxazoloisoindole, hinders microtubule assembly; effective against NCI cancer cells.</p>

<p>TPI 287: synthetic taxane; may halt cancer by stabilizing microtubules, blocking cell division, inducing apoptosis.</p>

<p>Compound 24: Potent Nrf2/HO-1 activator with neuroprotective, antioxidant properties; useful in PD research.</p>

<p>Tubulin-IN-35 inhibits oxazolylisoindole microtubule formation, targeting VL51 marginal zone lymphoma.</p>

<p>Onalespib lactate is a second-generation, potent and selective HSP90 Inhibitor with antitumor activity.</p>

<p>Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor that binds to the colchicine site on tubulin, causing G2/M cell cycle arrest and inducing reactive oxygen species (ROS) production. It demonstrates significant inhibitory activity against P-glycoprotein (P-gp) overexpressing cell lines MCF7/ADR and KBV200, with resistance indices (DRI) of 0.83 and 0.58, respectively. In an MCF-7 xenograft model, Antitumor agent-200 (at 25 mg/kg, administered intraperitoneally) achieves a 57.2% tumor growth inhibition rate. This compound is applicable for research in the field of cancer therapy.</p>

<p>Tubulin inhibitor 49 (Compound 18) is an inhibitor of tubulin polymerization with an IC50 of 48 μM. It disrupts the microtubule network of cells, causing cell cycle arrest in the G2 phase, and exhibits cytotoxicity with an IC50 of 8.8 μM in HeLa cells.</p>

<p>Quinagolide hydrochloride is a selective agonist of dopamine D2 receptor.</p>

<p>XD23 is a potent osteosarcoma inhibitor that functions by downregulating DKK1 and activating the WNT/β-catenin signaling pathway.</p>

<p>HSP90-IN-9: potent HSP90 inhibitor, dose-dependent fungicide, impedes biofilm/morphology with FLC, reverses FLC resistance.</p>

<p>AChE/GSK-3β-IN-1 is a potent dual AChE/GSK-3β inhibitor that crosses the blood-brain barrier and acts on hAChE (IC50: 1.2 nM), hBChE (IC50: 149.8 nM) and hGSK-</p>

<p>SPA0355 is a thiourea derivative with antioxidant and anti-inflammatory properties. It inhibits RANKL (receptor activator of nuclear factor κB ligand)-induced osteoclastogenesis in primary bone marrow-derived macrophages and suppresses the activation of MAPKs, Akt, and NF-κB pathways. Furthermore, SPA0355 enhances osteoblast differentiation by increasing alkaline phosphatase activity and mineralized nodule formation. It protects ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it a potential candidate for studying postmenopausal osteoporosis.</p>

<p>SF0166: potent αvβ3 antagonist, IC50: 0.6 nM. Blocks cell adhesion, IC50: 7.6 pM-76 nM. Reduces neovascularization in mice.</p>

<p>HSN748 is an analog of ponatinib and acts as a multi-kinase inhibitor. It exhibits inhibitory activity against kinases such as FLT3, ABL1, RET, PDGFRα/β, MNK1, and MNK2. HSN748 can suppress the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines, making it a useful compound in leukemia research.</p>

<p>Ethaboxam is a β-tubulin inhibitor and antifungal agent used against oomycete pathogens.</p>

<p>AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin Homology (PH) domain of AKT. It is useful for research related to cell proliferation and cancer involving the AKT pathway.</p>

<p>Hsp90-IN-38 (compound 20m) is an inhibitor of HSP90 (heat shock protein). It demonstrates a strong binding affinity to HSP90 with a Kd of 87 nM. The compound inhibits ATPase activity with an IC50 of 0.13 μM. Hsp90-IN-38 also shows inhibitory effects on HCT116, MCF-7, SKBr3, K562, and A549 cells with IC50 values of 0.187, 0.072, 0.105, 0.403, and 0.031 μM, respectively.</p>

<p>NAP1051, a biomimetic analog of Lipoxin A4, serves an anti-tumor role by targeting the inflammatory tumor microenvironment. It inhibits the chemotaxis of neutrophils to fMLP and stimulates macrophage efferocytosis by activating AKT. NAP1051 is utilized in research on colorectal cancer.</p>

<p>Tubulin polymerization-IN-77 (Compound 15c) is a microtubule polymerization inhibitor that exhibits anti-glioblastoma activity by hindering microtubule polymerization. It demonstrates significant blood-brain barrier permeability, effectively induces G2/M phase arrest in GBM cells, and triggers apoptosis, while also markedly inhibiting tumor cell migration.</p>

<p>Terpendole E is an atypical L5 site inhibitor.</p>

<p>KU-32 is a novel and novobiocin-based Hsp90 inhibitor. It can protect against neuronal cell death.</p>

<p>JC168 is a phenyl analog of peloruside and functions as a microtubule inhibitor with antiproliferative and anticancer properties. It enhances tubulin polymerization, thereby disrupting microtubule dynamics, making it a useful agent in the study of microtubule-associated diseases.</p>

<p>APN/AKT-IN-1, a dual APN (IC50=0.21μM) &amp; AKT (IC50=0.27μM) inhibitor, hinders GSK3β phosphorylation.</p>

<p>Si306, an Src inhibitor, exhibits antitumor activity by reducing the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM).</p>

<p>Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.</p>

<p>Myoseverin B is a microtubule assembly inhibitor that impedes tubulin polymerization (IC50 = 2 μM) and generally exhibits low cytotoxicity across most cell types. It is utilized in antitumor agent research.</p>

<p>β-Catenin modulator-8 (Compound Ⅸa) is a specific β-catenin modulator for use in cancer research.</p>

<p>Epothilone E, a derivative of epothilone, functions by inhibiting microtubule protein activity, thereby halting cell division and exhibiting anti-tumor</p>